Pharmacokinetics and biotransformation of benzbromarone in man.

After administration of a single oral dose of benzbromarone 100 mg to 7 subjects, the maximum serum level was 1.84 +/- 0.87 mg/l, and the elimination halflife was 2.77 +/- 1.07 h. The major metabolite, benzarone, could be detected in serum 3 h after administration of benzbromarone, and the maximum serum benzarone level of 0.79 +/- 0.21 mg/l occurred after 6 h. Benzarone had an elimination half-life from serum of 13.52 +/- 2.18 h. Both substances were excreted mainly via the liver and bile. In urine only benzarone beta-glucuronide could be detected; it amounted to 1.55% of the benzbromarone dose.